Pyridostatins selectively recognize two different forms of the human telomeric G-quadruplex structures and their anti-tumor activities in vitro
Wang, Li-Xia; Shang, Qian; Li, Qian; Xiang, Jun-Feng; Liu, Yan; Guan, Ai-Jiao; Sun, Hong-Xia; Yu, Li-Jia; Tang, Ya-Lin
刊名TETRAHEDRON
2015-07-29
卷号71期号:30页码:4982-4986
关键词G-quadruplex Recognition Stabilization Pyridostatin derivatives Anti-cancer drug
英文摘要G-quadruplex as a therapeutic target to develop novel anti-cancer agents has attracted a growing interest. Among all the ligands of G-quadruplexes, pyridostatin derivatives play a very important role. Here, we first reported the recognition of the fundamental skeleton pyridostatin I, which was simply synthesized. Compared to pyridostatin II comprising terminal amino groups, pyridostatin I selectively stabilized intramolecular anti-parallel telomeric G-quadruplex by raising the melting temperature about 20 degrees C at 295 rim of H22, while pyridostatin II preferred to stabilize intermolecular parallel telomeric G-quadruplex by raising the melting temperature about 25 degrees C at 265 nm of H7, maybe due to the suited size measurements between G-quadruplex hosts and pyridostatin guests. MTT assays indicated that pyridostatin II had better cytotoxic effects against HCT-8 and A549 cell lines obviously, indicating positively charged side chains may be required for improving the water solubility and cellular uptake of the apolar central skeleton. (C) 2015 Published by Elsevier Ltd.
收录类别SCI
语种英语
公开日期2015-10-27
内容类型期刊论文
源URL[http://ir.iccas.ac.cn/handle/121111/27806]  
专题化学研究所_分子动态与稳态结构实验室
作者单位Chinese Acad Sci, Inst Chem, State Key Lab Struct Chem Unstable & Stable Speci, Ctr Mol Sci,Beijing Natl Lab Mol Sci, Beijing 100190, Peoples R China
推荐引用方式
GB/T 7714
Wang, Li-Xia,Shang, Qian,Li, Qian,et al. Pyridostatins selectively recognize two different forms of the human telomeric G-quadruplex structures and their anti-tumor activities in vitro[J]. TETRAHEDRON,2015,71(30):4982-4986.
APA Wang, Li-Xia.,Shang, Qian.,Li, Qian.,Xiang, Jun-Feng.,Liu, Yan.,...&Tang, Ya-Lin.(2015).Pyridostatins selectively recognize two different forms of the human telomeric G-quadruplex structures and their anti-tumor activities in vitro.TETRAHEDRON,71(30),4982-4986.
MLA Wang, Li-Xia,et al."Pyridostatins selectively recognize two different forms of the human telomeric G-quadruplex structures and their anti-tumor activities in vitro".TETRAHEDRON 71.30(2015):4982-4986.
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